Lippold B C, Lettenbauer W A
Pharmazie. 1980;35(10):612-20.
The pharmaceutical-technological measure of varied salt formation acts on the in vivo diffusion processes of quaternary tridihexethyl (gastro-intestinal absorption, transperitoneal diffusion) in principle in the same manner as it acts on the in vitro diffusion processes (membrane diffusion): Due to the formation of corresponding ion pairs, lipophilic counterions of opposite sign facilitate the passage through membranes. In contrast, the direct pharmacodynamic activity (spasmolysis at the isolated jejunum of the rat) is not changed by varying the counterions of opposite sign.
形成不同盐类的药物技术措施对季铵类曲地铵在体内的扩散过程(胃肠道吸收、经腹膜扩散)的作用原理,与它对体外扩散过程(膜扩散)的作用原理相同:由于形成了相应的离子对,带相反电荷的亲脂性抗衡离子有助于药物透过膜。相比之下,改变带相反电荷的抗衡离子并不会改变其直接的药效学活性(对大鼠离体空肠的解痉作用)。